N-aryl heterocycles via coupling reactions with arylboronic acids

被引：104

作者：

Mederski, WWKR ^{[1
]}

Lefort, M ^{[1
]}

Germann, M ^{[1
]}

Kux, D ^{[1
]}

机构：

[1] Merck KGaA, Preclin Pharmceut Res, D-64271 Darmstadt, Germany

来源：

TETRAHEDRON | 1999年 / 55卷 / 44期

关键词：

arylation; coupling reactions; indoles; pyridazinones; pyridones; pyrroles;

D O I：

10.1016/S0040-4020(99)00752-8

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Compounds having a partial 2-pyridone structure or 3-pyridazinones can be selectively N-arylated with phenylboronic acids according to the procedure described by Chan and Lam. This procedure leads to N5-arylated imidazo[4,5-c]pyridin-4-ones, precursors of potent factor Xa inhibitors. In addition, the synthesis of N-aryl substituted pyrrole- and indole-2-carboxylic acid esters is described In the indole series this procedure offers a flexible entry in the synthesis of different 1,3-diaryl-2-carboxyindoles. (C) 1999 Elsevier Science Ltd. Ail rights reserved.

引用

页码：12757 / 12770

页数：14

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